• Starting from the hypothesis that the linker portion

  2022-06-22

  

  Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [

• Importantly HDACi mediated effects are cell and

  2022-06-22

  

  Importantly, HDACi-mediated effects are cell and HDAC specific; different effects and outcomes have been observed in different cell types, targeting different HDAC isoforms. While HDACi exhibit a strong proapoptotic potential in human leukemia 96 7 19, 20, 21, 22, they have a limited ability to ind

• Main Text There are over small GTPases that play

  2022-06-22

  

  Main Text There are over 200 small GTPases that play critical roles in diverse fundamental cellular processes such as signal transduction, NSC 207895 dynamics, and intracellular trafficking. Most of the GTPases act as switch-like molecules by cycling between the guanosine triphosphate (GTP)-bound “

• Accessibility and physico chemical features of

  2022-06-22

  

  Accessibility and physico-chemical features of cysteine residues define their redox-reactivity and the 3-dimensional structure of GSNOR allows to identifying such surface-exposed, redox-sensitive cysteine residues. GSNOR crystal structures are available from human (Protein Data Bank code: 1MP0), tom

• Glycogen synthase kinase GSK is an evolutionarily conserved

  2022-06-22

  

  Glycogen synthase kinase-3β (GSK-3β) is an evolutionarily conserved serine/threonine kinase that plays multifaceted role in diverse cellular and neurophysiological processes [8]. GSK-3β is regulated by inhibitory serine and stimulatory tyrosine phosphorylation on Ser9 and Tyr216 respectively [9]. Dy

• Continuing studies of endocannabinoid ligands at GPR reveal

  2022-06-21

  

  Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort

• 11-dUTP br Author contributions br Acknowledgements

  2022-06-21

  

  Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa

• Transporters are important ta http www apexbt com

  2022-06-21

  

  Transporters are important targets for devising new therapies, optimizing existing therapies, and helping understand the toxicities of certain drugs. Given the well-documented role of transporters in restricting the distribution of drugs, modulating the relevant transporters could enhance the permea

• Inhibitors against the proteasome a component

  2022-06-21

  

  Inhibitors against the proteasome, a component of the ubiquitin-proteasome pathway that degrades cellular proteins, provide a new strategy for targeting the 26S proteasome [25]. Proteasome inhibitors can exhibit potent anti-cancer effects against different tumor RI-1 and were shown to induce apoptos

• Of note the intracellular egg compartment exhibiting SA gal

  2022-06-21

  

  Of note, the intracellular egg compartment exhibiting SA-β-gal activity also exhibits lipofuscin auto-fluorescence (Fig. 6B), and it is co-stained with the lipid-specific dye SBB (Supplemental Fig. 5). On the one hand, these findings reflect the fact that the pool of yolk protein contains lipoprotei

• Corresponding to the different insulinotropic signaling the

  2022-06-21

  

  Corresponding to the different insulinotropic signaling, the competitive radioligand-binding studies demonstrated at least 3 distinct Autophagy Compound Library on GPR40: orthosteric binding site for endogenous ligands, allosteric binding site for partial agonists and another allosteric binding site

• To meet the requirement of ferroptosis based therapy a

  2022-06-21

  

  To meet the requirement of ferroptosis-based therapy, a couple of small molecule drugs and nanomaterials were introduced to the design of ferroptosis inducers, separately. As we know, iron is a key regulator of ferroptosis. When small molecule drugs are employed to induce ferroptosis, the endogenous

• One of the main mechanisms

  2022-06-21

  

  One of the main mechanisms enabling recycling of intracellular redox-active iron is lysosomal degradation of ferritin in the process of autophagy, often referred to as ‘ferritinophagy’ [128]. Autophagy was suggested to contribute to ferroptotic cell death by promoting the degradation of iron storage

• During the activation of the coagulation cascade factor

  2022-06-21

  

  During the activation of the coagulation cascade, factor Xa (FXa) forms a complex with activated factor V and calcium VX-702 on the surface of platelet membrane (so called prothrombinase complex) and converts prothrombin to thrombin [5], [6]. Selective FXa inhibitors do not directly inhibit platele

• luteolin Following the discovery of diketo compounds

  2022-06-20

  

  Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent luteolin based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioas

16460 records 438/1098 page Previous Next First page 上5页 436437438439440 下5页 Last page